Abstract

The 46th EuroCongress on Drug Synthesis and Analysis (ECDSA-2017) was arranged within the celebration of the 65th Anniversary of the Faculty of Pharmacy at Comenius University in Bratislava, Slovakia from 5–8 September 2017 to get together specialists in medicinal chemistry, organic synthesis, pharmaceutical analysis, screening of bioactive compounds, pharmacology and drug formulations; promote the exchange of scientific results, methods and ideas; and encourage cooperation between researchers from all over the world. The topic of the conference, “Drug Synthesis and Analysis,” meant that the symposium welcomed all pharmacists and/or researchers (chemists, analysts, biologists) and students interested in scientific work dealing with investigations of biologically active compounds as potential drugs. The authors of this manuscript were plenary speakers and other participants of the symposium and members of their research teams. The following summary highlights the major points/topics of the meeting.

Highlights

  • As the research of fangchinoline moved along, along, we found that fangchinoline could induce human hepatocellular carcinoma cells (HCC) death we found that fangchinoline could induce human hepatocellular carcinoma cells (HCC) death through through an autophagic mechanism by inducing translocation of p53 and activating AMPK, which is an autophagic mechanism by inducing translocation of p53 and activating AMPK, which is totally totally different of tetrandrine [37]

  • 9-cis-Retinoic acid, which is synthesized primarily intracellularly from retinaldehyde that can be produced from β-carotene, induced macrophage cholesterol efflux via the LXRα-dependent up-regulation of ATP-binding cassette transporter A1 (ABCA1) and ABCG1 [17]. 9-cis-Retinoic acid reduced the atherosclerotic plaque area in the aortic sinus of apolipoprotein E (apoE)−/− mice [119]. 9-cis-β-carotene, a precursor for 9-cis-Retinoic-acid, as well as all-trans-β-carotene significantly increased cholesterol efflux from RAW264.7 macrophages, which might be ascribed to transcriptional induction of ABCA1, ABCG1, and apoE [120]

  • Natural products from traditional medicine and food represent an important pool for the identification of compounds with cholesterol efflux enhancing capacity

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Summary

Introduction

According to the latest WHO Global Tuberculosis Report, estimated 10.4 million people worldwide developed active tuberculosis (TB) in 2015 [86]. Intracellular accumulation of POA leads to acidification of cytoplasm, disruption of membrane potentials and interferes with processes dependent on proton gradient [88]. In 2015, this non-specific MoA was challenged by Peterson et al [89], who directly measured the intracellular pH of mycobacterial cells cultivated with PZA or POA. They observed only minor, probably biologically irrelevant, acidification after prolonged cultivation with.

Finding In-silico Paradise in Multidimensional QSAR Studies
Illustration
En Route to New Anticancer Agents Based on Alkaloid Luotonin A
Structures
Targeting Oncogenic Mutant TP53—One Step Ahead
Non-Canonical Cell Death Mechanisms as a Pharmacological Target
Inhibition of Fatty Acid Synthase Type I
Inhibition of Trans-Translation
Other Specific Targets for PZA
Implications for Structure-Based Drug Design
10.1. Introduction
10.2. Flavonoids and Polyphenols
10.3. Carotene and Its Derivatives
10.4. Fatty Acids
10.5. Other Compounds
10.6. Conclusions
11.1. Introduction
11.2. Design of Novel Ligands
11.3. Conclusions
Chemical
12. Synthesis
13. Biomimetic Chromatography as a User-Friendly Technique in Drug Discovery
14.1. Introduction
14.3. Chromatography in Enantioreolution and Enantioseparation of α-Amino Acids
14.4. Discovery of Spontaneous Oscillatory Reactions
Conclusions
15. Towards Complete Identification of Drugs of Abuse
Jendrzejewska
11. Diffraction
12. Comparison ofofcalculated values ofofdhkl with values found in the
Findings
17. Big Data Problem in Drug Design
Full Text
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